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mAChR

Muscarinic acetylcholine receptors (mAChRs) are a class of G protein-coupled receptors (GPCRs) found in the central and peripheral nervous systems, as well as in various other tissues and organs throughout the body. These receptors are named after muscarine, a natural alkaloid compound found in certain mushrooms, which was one of the first substances discovered to activate them.

There are five subtypes of muscarinic receptors, designated as M1 through M5, each with distinct tissue distribution and functions. Here's an overview of their roles:

  • M1 Receptors: Predominantly found in the central nervous system, particularly in regions associated with cognitive functions. Activation of M1 receptors is linked to memory and learning.
  • M2 Receptors: Found in the heart, where they play a crucial role in regulating heart rate and cardiac contractility. Activation of M2 receptors slows heart rate and reduces the force of cardiac contractions.
  • M3 Receptors: Present in smooth muscle tissues, such as those in the gastrointestinal tract, urinary bladder, and bronchial airways. Activation of M3 receptors leads to smooth muscle contraction.
  • M4 Receptors: Distributed mainly in the central nervous system and involved in modulating neurotransmitter release. Their role in cognition and neuropsychiatric disorders is of interest.
  • M5 Receptors: Located in certain areas of the brain and implicated in the modulation of dopamine release. Research suggests they may be relevant to Parkinson's disease and addiction.

Muscarinic receptors are activated by the neurotransmitter acetylcholine and play a vital role in regulating a wide range of physiological processes, including heart rate, smooth muscle contraction, glandular secretion, and neurotransmitter release. They are targets for various drugs, including anticholinergic agents, which block their activity, and drugs used to treat conditions like bradycardia and neurodegenerative disorders.

Understanding the functions and regulation of muscarinic acetylcholine receptors is essential for developing therapies that modulate their activity and for advancing our knowledge of how they contribute to various physiological and pathological processes in the body.

Items 1-25 of 167

  • Atropine sulfate monohydrate
    Cat. No.
    A10098
    CAS No.
    5908-99-6

    Atropine sulfate monohydrate

    Synonyms: Atropisol; Atropt; Atropini sulfas; Tropine tropate

    Atropine is a competitive antagonist for the muscarinic acetylcholine receptor types M1, M2, M3, M4 and M5.

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    50 mg
    $20.00
    100 mg
    $25.00
    All 3 sizes
  • Biperiden HCl
    Cat. No.
    A10147
    CAS No.
    1235-82-1

    Biperiden HCl

    Synonyms: Akineton

    Biperiden hydrochloride is a muscarinic receptor antagonist that displays some selectivity for the M1 subtype

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    5 mg
    $90.00
    10 mg
    $150.00
    All 5 sizes
  • Fesoterodine fumarate
    Cat. No.
    A10386
    CAS No.
    286930-03-8

    Fesoterodine fumarate

    Synonyms: Toviaz

    Fesoterodine fumarate is a medicine which is used in urinary urgency, reducing the frequency of passing urine and urge urinary incontinence

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    2 mg
    $30.00
    5 mg
    $45.00
    All 8 sizes
  • Ipratropium bromide
    Cat. No.
    A10476
    CAS No.
    22254-24-6

    Ipratropium bromide

    Synonyms: Atrovent; Apovent; Aerovent

    Ipratropium bromide is a muscarinic antagonist, bronchodilator, N-Isopropyl salt of atropine.

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    25 mg
    $20.00
    50 mg
    $35.00
    All 7 sizes
  • Tiotropium Bromide
    Cat. No.
    A10934
    CAS No.
    136310-93-5

    Tiotropium Bromide

    Synonyms: BA679 BR; BA 679

    Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.

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    5 mg
    $30.00
    10 mg
    $30.00
    All 7 sizes
  • Trospium chloride
    Cat. No.
    A10951
    CAS No.
    10405-02-4

    Trospium chloride

    Trospium chloride is a selective and competitive antagonist of muscarinic acetylcholine receptors (mAChRs). It exhibits potent antimuscarinic activity by binding with high affinity to M1, M2, and M3 receptor subtypes, while showing no interaction with nicotinic cholinergic receptors. This compound is primarily utilized in research related to neurological conditions and to explore the pharmacological modulation of cholinergic signaling.

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    100 mg
    $25.00
    500 mg
    $45.00
    All 3 sizes
  • Quifenadine
    Cat. No.
    A11114
    CAS No.
    10447-39-9

    Quifenadine

    Quifenadine is a potent M3 receptor antagonist, exhibiting an IC50 value greater than 1000 nM. This compound is valuable for research into neurological diseases and related conditions. It serves as a tool for studying the role of M3 receptors in various biological systems and may contribute to the development of therapeutic strategies targeting these pathways.

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    10 mg
    $340.00
    100 mg
    $2,510.00
    All 2 sizes
  • Solifenacin succinate
    Cat. No.
    A11215
    CAS No.
    242478-38-2

    Solifenacin succinate

    Synonyms: YM905; Vesicare

    Solifenacin-succinate is a muscarinic M3 receptor antagoinst, used in treatment of urinary incontinence.

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    10 mg
    $20.00
    50 mg
    $25.00
    All 6 sizes
  • Darifenacin hydrobromide
    Cat. No.
    A11391
    CAS No.
    133099-07-7

    Darifenacin hydrobromide

    Synonyms: UK-88525 hydrobromide

    Darifenacin (UK-88525) hydrobromide is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin hydrobromide binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin hydrobromide can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin hydrobromide inhibits tumor growth in colorectal cancer cells and has anti-tumor effects.

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    5 mg
    $20.00
    10 mg
    $25.00
    All 6 sizes
  • Orphenadrine citrate
    Cat. No.
    A11712
    CAS No.
    4682-36-4

    Orphenadrine citrate

    Synonyms: Norflex

    Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.

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    50 mg
    $20.00
    100 mg
    $25.00
    All 5 sizes
  • Oxybutynin chloride
    Cat. No.
    A11899
    CAS No.
    1508-65-2

    Oxybutynin chloride

    Oxybutynin chloride is a competitive antagonist of muscarinic acetylcholine receptors (mAChRs), exhibiting binding affinities with Ki values of 14.3 nM and 5.55 nM for [3H]NMS in mouse bladder and cerebral cortex, respectively. It effectively inhibits vascular Kv channels with an IC50 of 11.51 μM, independent of its anticholinergic effects. Oxybutynin chloride is primarily utilized for the management of overactive bladder syndrome (OAB) and alleviating bladder and urinary tract muscle spasms. Additionally, it serves as a click chemistry reagent due to its alkyne functionality, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules.

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    100 mg
    $25.00
    500 mg
    $45.00
    All 4 sizes
  • Beperidium iodide
    Cat. No.
    A12382
    CAS No.
    86434-57-3

    Beperidium iodide

    Synonyms: SX 810

    Beperidium iodide shows a competitive antagonistic effect against acetylcholine receptor with a pA2 of 7.93.

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    1 mg
    $85.00
    5 mg
    $345.00
    All 6 sizes
  • Glycopyrrolate
    Cat. No.
    A12641
    CAS No.
    596-51-0

    Glycopyrrolate

    Synonyms: Glycopyrrolate bromide; Glycopyrronium bromide

    Glycopyrrolate is a muscarinic competitive antagonist used as an antispasmodic.

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    5 mg
    $25.00
    10 mg
    $35.00
    All 7 sizes
  • Flavoxate
    Cat. No.
    A12900
    CAS No.
    15301-69-6

    Flavoxate

    Synonyms: BML-278; Urispas; Bladuril; Spasuret; Uronid

    Flavoxate binds and inhibits muscarinic receptors, thereby suppressing the micturition reflex and increases urinary bladder capacity by modifying the micturition center in the brain stem.

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    10 mg
    $70.00
    25 mg
    $145.00
    All 3 sizes
  • AF-DX 384
    Cat. No.
    A13856
    CAS No.
    118290-26-9

    AF-DX 384

    AF-DX 384 is a drug which acts as a selective antagonist of the muscarinic acetylcholine receptors.

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    1 mg
    $75.00
    5 mg
    $200.00
    All 5 sizes
  • Atropine methyl nitrate
    Cat. No.
    A13857
    CAS No.
    52-88-0

    Atropine methyl nitrate

    Synonyms: Methylatropine nitrate

    Atropine methyl nitrate is a muscarinic acetylcholine receptor (mAChR) antagonist, primarily utilized for its ability to induce pupil dilation (mydriasis) during ophthalmic examinations. This quaternary ammonium derivative is specifically formulated for the treatment of pyloric spasms in infants due to its high polarity, which limits its central nervous system penetration compared to its parent compound, atropine. Research applications include studying cholinergic signaling pathways and exploring therapeutic strategies for gastrointestinal disorders.

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    5 mg
    $130.00
    10 mg
    $215.00
    All 5 sizes
  • Diphenidol HCl
    Cat. No.
    A14244
    CAS No.
    3254-89-5

    Diphenidol HCl

    Diphenidol HCl is a potent antagonist of muscarinic M2 and M3 receptor with pKb of 6.72 and 7.02.

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    100 mg
    $40.00
    200 mg
    $60.00
    All 4 sizes
  • Umeclidinium bromide
    Cat. No.
    A15268
    CAS No.
    869113-09-7

    Umeclidinium bromide

    Synonyms: GSK573719A

    Umeclidinium bromide(GSK573719A) is a muscarinic receptor antagonist which is useful in treatment of chronic obstructive pulmonary disease (COPD).

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    1 mg
    $25.00
    2 mg
    $40.00
    All 8 sizes

Items 1-25 of 167

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